Stem definition | Drug id | CAS RN |
---|---|---|
Hepatitis Virus C (HVC) protease inhibitors | 4812 | 923604-59-5 |
Dose | Unit | Route |
---|---|---|
0.15 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
May 14, 2014 | EMA | ||
Nov. 22, 2013 | FDA | JANSSEN PRODS |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Platelet count decreased | 761.49 | 35.46 | 301 | 4414 | 100425 | 50499984 |
Anaemia | 561.84 | 35.46 | 325 | 4390 | 252131 | 50348278 |
White blood cell count decreased | 460.22 | 35.46 | 221 | 4494 | 116501 | 50483908 |
Blood bilirubin increased | 380.59 | 35.46 | 134 | 4581 | 31904 | 50568505 |
Neutrophil count decreased | 275.48 | 35.46 | 117 | 4598 | 45909 | 50554500 |
Haemoglobin decreased | 211.83 | 35.46 | 137 | 4578 | 127079 | 50473330 |
Hyperbilirubinaemia | 164.68 | 35.46 | 53 | 4662 | 9517 | 50590892 |
Haemolytic anaemia | 145.84 | 35.46 | 48 | 4667 | 9244 | 50591165 |
Hepatitis C | 108.72 | 35.46 | 33 | 4682 | 4884 | 50595525 |
Hepatocellular carcinoma | 107.63 | 35.46 | 27 | 4688 | 1972 | 50598437 |
Pruritus | 103.10 | 35.46 | 129 | 4586 | 283439 | 50316970 |
Off label use | 102.17 | 35.46 | 168 | 4547 | 474258 | 50126151 |
Pyrexia | 91.80 | 35.46 | 142 | 4573 | 380061 | 50220348 |
Photosensitivity reaction | 84.29 | 35.46 | 35 | 4680 | 12876 | 50587533 |
Remission not achieved | 52.61 | 35.46 | 9 | 4706 | 94 | 50600315 |
Decreased appetite | 45.38 | 35.46 | 73 | 4642 | 200850 | 50399559 |
Hepatic failure | 42.08 | 35.46 | 30 | 4685 | 32253 | 50568156 |
Hepatic function abnormal | 41.75 | 35.46 | 30 | 4685 | 32651 | 50567758 |
Jaundice | 40.18 | 35.46 | 27 | 4688 | 26402 | 50574007 |
Sunburn | 40.04 | 35.46 | 13 | 4702 | 2390 | 50598019 |
Hepatic encephalopathy | 39.93 | 35.46 | 19 | 4696 | 9617 | 50590792 |
Hepatitis C RNA increased | 37.37 | 35.46 | 7 | 4708 | 126 | 50600283 |
Depressive symptom | 36.39 | 35.46 | 13 | 4702 | 3187 | 50597222 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Platelet count decreased | 543.91 | 28.88 | 300 | 5265 | 104372 | 29464590 |
White blood cell count decreased | 391.23 | 28.88 | 224 | 5341 | 83138 | 29485824 |
Blood bilirubin increased | 351.15 | 28.88 | 156 | 5409 | 33737 | 29535225 |
Anaemia | 309.56 | 28.88 | 273 | 5292 | 200678 | 29368284 |
Hepatitis C | 286.94 | 28.88 | 94 | 5471 | 8816 | 29560146 |
Hepatocellular carcinoma | 254.09 | 28.88 | 81 | 5484 | 6957 | 29562005 |
Off label use | 214.24 | 28.88 | 271 | 5294 | 300529 | 29268433 |
Hyperbilirubinaemia | 171.31 | 28.88 | 74 | 5491 | 14860 | 29554102 |
Neutrophil count decreased | 144.17 | 28.88 | 94 | 5471 | 43473 | 29525489 |
Haemoglobin decreased | 143.66 | 28.88 | 136 | 5429 | 108239 | 29460723 |
Photosensitivity reaction | 140.34 | 28.88 | 56 | 5509 | 9202 | 29559760 |
Drug ineffective | 95.94 | 28.88 | 210 | 5355 | 362960 | 29206002 |
Jaundice | 72.67 | 28.88 | 53 | 5512 | 29243 | 29539719 |
Remission not achieved | 71.77 | 28.88 | 13 | 5552 | 89 | 29568873 |
Pruritus | 69.47 | 28.88 | 97 | 5468 | 116752 | 29452210 |
Haemolytic anaemia | 59.56 | 28.88 | 31 | 5534 | 9388 | 29559574 |
Sunburn | 51.69 | 28.88 | 17 | 5548 | 1603 | 29567359 |
Treatment failure | 49.93 | 28.88 | 47 | 5518 | 36892 | 29532070 |
Hepatic failure | 46.27 | 28.88 | 42 | 5523 | 31470 | 29537492 |
Genotype drug resistance test positive | 46.22 | 28.88 | 14 | 5551 | 1009 | 29567953 |
Pyrexia | 44.99 | 28.88 | 137 | 5428 | 287485 | 29281477 |
Ascites | 44.59 | 28.88 | 44 | 5521 | 36575 | 29532387 |
Viral load increased | 44.02 | 28.88 | 16 | 5549 | 2033 | 29566929 |
Hepatitis C RNA increased | 42.38 | 28.88 | 10 | 5555 | 274 | 29568688 |
Hepatic encephalopathy | 40.27 | 28.88 | 27 | 5538 | 13008 | 29555954 |
Thought blocking | 38.29 | 28.88 | 8 | 5557 | 123 | 29568839 |
Bilirubin conjugated increased | 38.01 | 28.88 | 16 | 5549 | 3001 | 29565961 |
Rash | 34.96 | 28.88 | 96 | 5469 | 189723 | 29379239 |
Choroiditis | 34.08 | 28.88 | 11 | 5554 | 977 | 29567985 |
Hyperuricaemia | 33.34 | 28.88 | 19 | 5546 | 6870 | 29562092 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Platelet count decreased | 1351.13 | 29.50 | 600 | 8987 | 167111 | 64322034 |
White blood cell count decreased | 894.43 | 29.50 | 444 | 9143 | 157393 | 64331752 |
Anaemia | 846.23 | 29.50 | 581 | 9006 | 378099 | 64111046 |
Blood bilirubin increased | 681.15 | 29.50 | 272 | 9315 | 57281 | 64431864 |
Neutrophil count decreased | 414.02 | 29.50 | 210 | 9377 | 76986 | 64412159 |
Hepatitis C | 384.83 | 29.50 | 117 | 9470 | 10898 | 64478247 |
Haemoglobin decreased | 357.77 | 29.50 | 267 | 9320 | 194796 | 64294349 |
Hepatocellular carcinoma | 357.69 | 29.50 | 104 | 9483 | 8299 | 64480846 |
Hyperbilirubinaemia | 313.32 | 29.50 | 118 | 9469 | 21087 | 64468058 |
Haemolytic anaemia | 200.18 | 29.50 | 79 | 9508 | 15974 | 64473171 |
Pruritus | 156.28 | 29.50 | 211 | 9376 | 312189 | 64176956 |
Photosensitivity reaction | 138.31 | 29.50 | 63 | 9524 | 18110 | 64471035 |
Pyrexia | 136.87 | 29.50 | 273 | 9314 | 558371 | 63930774 |
Jaundice | 105.75 | 29.50 | 74 | 9513 | 48438 | 64440707 |
Remission not achieved | 104.73 | 29.50 | 21 | 9566 | 335 | 64488810 |
Off label use | 103.00 | 29.50 | 263 | 9324 | 632543 | 63856602 |
Hepatic failure | 81.88 | 29.50 | 67 | 9520 | 55327 | 64433818 |
Hepatic encephalopathy | 65.10 | 29.50 | 40 | 9547 | 21026 | 64468119 |
Rash | 62.64 | 29.50 | 179 | 9408 | 458370 | 64030775 |
Hepatitis C RNA increased | 62.53 | 29.50 | 14 | 9573 | 386 | 64488759 |
Bilirubin conjugated increased | 60.32 | 29.50 | 24 | 9563 | 4944 | 64484201 |
Ascites | 56.20 | 29.50 | 57 | 9530 | 61944 | 64427201 |
Pain | 55.92 | 29.50 | 8 | 9579 | 553503 | 63935642 |
Hyperuricaemia | 55.23 | 29.50 | 28 | 9559 | 10163 | 64478982 |
Sunburn | 54.48 | 29.50 | 20 | 9567 | 3312 | 64485833 |
Decreased appetite | 52.97 | 29.50 | 124 | 9463 | 281165 | 64207980 |
Insomnia | 48.42 | 29.50 | 97 | 9490 | 197739 | 64291406 |
Malaise | 47.69 | 29.50 | 148 | 9439 | 396099 | 64093046 |
Hepatorenal syndrome | 45.14 | 29.50 | 18 | 9569 | 3728 | 64485417 |
Aspartate aminotransferase increased | 43.78 | 29.50 | 70 | 9517 | 119718 | 64369427 |
Red blood cell count decreased | 41.15 | 29.50 | 43 | 9544 | 48343 | 64440802 |
Hepatic function abnormal | 40.72 | 29.50 | 49 | 9538 | 64264 | 64424881 |
Hepatic cirrhosis | 39.23 | 29.50 | 32 | 9555 | 26266 | 64462879 |
Viral load increased | 37.26 | 29.50 | 14 | 9573 | 2473 | 64486672 |
Thought blocking | 36.87 | 29.50 | 8 | 9579 | 190 | 64488955 |
Liver disorder | 36.01 | 29.50 | 42 | 9545 | 53309 | 64435836 |
Choroiditis | 35.60 | 29.50 | 11 | 9576 | 1076 | 64488069 |
Alanine aminotransferase increased | 31.41 | 29.50 | 66 | 9521 | 138965 | 64350180 |
Incorrect product administration duration | 31.35 | 29.50 | 19 | 9568 | 9739 | 64479406 |
Injection site dermatitis | 31.23 | 29.50 | 5 | 9582 | 19 | 64489126 |
None
Source | Code | Description |
---|---|---|
ATC | J05AP05 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections |
MeSH PA | D000890 | Anti-Infective Agents |
MeSH PA | D000998 | Antiviral Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D011480 | Protease Inhibitors |
FDA MoA | N0000182138 | Cytochrome P450 1A2 Inhibitors |
FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
FDA MoA | N0000182638 | HCV NS3/4A Protease Inhibitors |
FDA EPC | N0000182639 | Hepatitis C Virus NS3/4A Protease Inhibitor |
FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
FDA MoA | N0000190107 | Organic Anion Transporting Polypeptide 1B1 Inhibitors |
FDA MoA | N0000190108 | Organic Anion Transporting Polypeptide 1B3 Inhibitors |
FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
FDA MoA | N0000193845 | Bile Salt Export Pump Inhibitors |
FDA MoA | N0000193960 | Multidrug Resistance-Associated Protein 2 Inhibitors |
FDA MoA | N0000193965 | Sodium Taurocholate Co-transporting Polypeptide Inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Chronic hepatitis C | indication | 128302006 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 4.35 | acidic |
pKa2 | 6.66 | Basic |
pKa3 | 3.5 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8349869 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8741926 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8754106 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9040562 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9353103 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9623022 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 9856265 | July 28, 2026 | METHOD OF TREATING HEPATITIS C |
EQ 150MG BASE | OLYSIO | JANSSEN PRODS | N205123 | Nov. 22, 2013 | DISCN | CAPSULE | ORAL | 8148399 | Sept. 5, 2029 | METHOD OF TREATING HEPATITIS C |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Cathepsin S | Enzyme | IC50 | 6.10 | CHEMBL | |||||
Hepatitis C virus serine protease, NS3/NS4A | Enzyme | INHIBITOR | Ki | 9.30 | CHEMBL | CHEMBL | |||
Genome polyprotein | Polyprotein | INHIBITOR | Ki | 9.44 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Nonstructural protein NS3-4A | Unclassified | Ki | 9.44 | CHEMBL | |||||
Polyprotein | Polyprotein | INHIBITOR | Ki | 9.44 | IUPHAR | ||||
Genome polyprotein | Unclassified | Ki | 9.30 | CHEMBL |
ID | Source |
---|---|
D10081 | KEGG_DRUG |
1241946-89-3 | SECONDARY_CAS_RN |
4032900 | VANDF |
CHEBI:134743 | CHEBI |
30B | PDB_CHEM_ID |
CHEMBL501849 | ChEMBL_ID |
7367 | IUPHAR_LIGAND_ID |
9432 | INN_ID |
DB06290 | DRUGBANK_ID |
9WS5RD66HZ | UNII |
24873435 | PUBCHEM_CID |
1482790 | RXNORM |
207569 | MMSL |
29896 | MMSL |
d08182 | MMSL |
015309 | NDDF |
015310 | NDDF |
708823009 | SNOMEDCT_US |
714167009 | SNOMEDCT_US |
D000069616 | MESH_DESCRIPTOR_UI |
C2605855 | UMLSCUI |
CHEMBL3137358 | ChEMBL_ID |
None